Oxazepam (4a) has been used as overall starting material in the synthesis of novel 2-substituted 1,4-benzodiazepines.By reacting Oxazepam 4a with commercially available hydrazines, hydrazides, semicarbazide, aminoguanidine and N,N-dimethylamino aniline in ethanol under acetic conditions, a series of diazenyl-1,4-benzodiazepines 5aâ5i and 2-amino-1,4-benzodiazepine 5k were obtained in good yield...

The solvent-free preparation of unsymmetrical N-aryl-5,6-unsubstituted-1,4-dihydropyridines (DHPs) by ball-milling was investigated. Three different mechanochemical domino reactions (one-pot/one step or stepwise) were studied, the process parameters underlying any modulated and differences with solution-based mechanistic pathways disclosed. selection most suitable method driven physical state b...

Gold-catalysed, divergent synthesis of 2-sulfonylmethyl pyrroles and dihydropyridines from N-propargyl-N-vinyl sulfonamides has been achieved. Echavarren's gold(I) catalyst promoted the formation of pyrrole derivatives whereas the combination of PPh3AuCl and AgSbF6 afforded dihydropyridines. The aza-enyne precursors for the cycloisomerisation reaction were prepared by a base-mediated formal vin...

We present the design, synthesis and biological activity of novel N-substituted benzimidazole based acrylonitriles as potential tubulin polymerization inhibitors. Their was achieved using classical linear organic microwave assisted techniques, starting from aromatic aldehydes N-substituted-2-cyanomethylbenzimidazoles. All newly prepared compounds were tested for their antiproliferative in vitro...

When treated with difluorocarbene, which was generated from FSO2CF2CO2SiMe3 a 1,8-bis(dimethylamino)naphthalene catalyst, N-(thioacyl)amidines underwent [4 + 1] cycloaddition to afford the corresponding amino-substituted 5,5-difluorothiazolines. Both dehydrofluorination and Hofmann elimination/SN2?-type reaction sequence enabled aromatization of obtained products, affording 5-fluorothiazoles. T...

Abstract The enaminone, (2 E )-3-(dimethylamino)-1-(3,4,5-trimethoxyphenyl) prop-2-en-1-one was prepared by refluxing 3,4,5-trimethoxy acetophenone with dimethylformamide dimethylacetal (DMF–DMA) without solvent for 12 h. dihydropyrimidinone derivatives (1–9) were reacting substituted benzaldehydes and urea in glacial acetic acid. compounds synthesized significant yield using one step multicomp...

Cigarette mainstream smoke (MS) contains a number of structurally diverse substituted phenols. Recent quantitative structure activity relationship (QSAR) studies on phenols show that substituted phenols with electron-releasing groups can form potentially toxic phenoxyl-free radicals. In contrast, substituted phenols with electron-withdrawing groups do not form phenoxyl-free radicals but exert t...

Cobalt(II) and manganese(III) phthalocyanines bearing peripherally and non-peripherally tetra substituted {(2E)-3-[4-(dimethylamino)phenyl]prop-2-enoyl}phenoxy groups were synthesized by cyclotetramerization of the phthalonitrile derivatives and their electrochemical properties were examined using CV and SWV techniques for the first time. The novel compounds were characterized by using IR, (1)H...

DESCRIPTION ZITHROMAX (azithromycin tablets and azithromycin for oral suspension) contain the active ingredient azithromycin, an azalide, a subclass of macrolide antibiotics, for oral administration. Azithromycin has the chemical name (2R,3S,4R,5R,8R,10R,11R,12S,13S,14R)-13-[(2,6-dideoxy3-C-methyl-3-O-methyl-α-Lribo-hexopyranosyl)oxy]-2-ethyl-3,4,10-trihydroxy-3,5,6,8,10,12,14-heptamethyl-11-[[...